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- 2025年12月05日
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4°C, protect from light, stored under nitrogen
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货期：1-2天
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MedChemExpress LLC
- CAS号：
1799633-27-4
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥4087.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥990.0 |
| 规格： | 5 mg | 产品价格： | ￥2800.0 |
| 规格： | 10 mg | 产品价格： | ￥4480.0 |
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S63845
CAS No. : 1799633-27-4
MCE 国际站：S63845
产品活性：S63845 是一种有效的选择性骨髓细胞白血病 1 (MCL1) 抑制剂，结合人 MCL1 的 Kd 值为 0.19 nM。
研究领域：Apoptosis
作用靶点：Bcl-2 Family
In Vitro: The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM).
In Vivo: S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.
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